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Tocris/EC 144/4701/10/10 mg
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Tocris/EC 144/4701/10/10 mg
品牌 / 
Tocris
货号 / 
4701/10
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4000-520-616
Description:Highaffinity,potentandselectiveHsp90inhibitor
ChemicalName:5-[2-Amino-4-chloro-7-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-2-methyl-4-pentyn-2-ol
Purity:≥98%(HPLC)
BIOLOGicalActivityTechnicalDataSolubilityCalculatorsDatasheetsReferences

BiologicalActivity

Highaffinity,potentandselectiveHsp90inhibitor(Ki=0.2nMandIC50=1.1nM).ExhibitsselectivityforHsp90overGrp94andTRAP1(Kivaluesare61and255nMrespectively)andhasnoeffect(IC50>10μM)againstapanelof285kinases.DegradesHer-2inMCF-7breastcancercells(EC50=14nM).BlockstumorgrowthandinducespartialtumorregressioninanN87gastrictumormousemodel.AlsoinhibitsLPS-inducedTNFαreleaseinanLPSshockmousemodelandsuppressesdiseasedevelopmentinaratmodelofcollagen-inducedarthritis.Exhibits<20-foldefficacyoverBIIB021(Cat.No.4608)inmice.Orallyavailableandbrainpenetrant.

CompoundLibraries

EC144isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.

TechnicalData

M.Wt413.9
FormulaC21H24ClN5O2
StorageStoreat-20°C
Purity≥98%(HPLC)
CASNumber911397-80-3
PubChemID11517212
InChIKeyVOASEWXFCTZRDF-UHFFFAOYSA-N
SmilesClC1=C2C(N(CC3=C(C)C(OC)=C(C)C=N3)C=C2C#CCC(C)(C)O)=NC(N)=N1

Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.

AllTocrisproductsareintendedforlaboratoryresearchuseonly.

SolubilityData

SolventMaxConc.mg/mLMaxConc.mM
Solubility
DMSO41.39100

PreparingStockSolutions

Thefollowingdataisbasedontheproductmolecularweight413.9.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.

Concentration/SolventVolume/Mass1mg5mg10mg
1mM2.42mL12.08mL24.16mL
5mM0.48mL2.42mL4.83mL
10mM0.24mL1.21mL2.42mL
50mM0.05mL0.24mL0.48mL

ProductDatasheets

CertificateofAnalysis/ProductDatasheet
SafetyDatasheet